Diacylglycerol acyltransferase (DGAT) is a microsomal enzyme that plays a central role in the metabolism of cellular glycerolipids. DGAT catalyzes the final step in triacylglycerol (TAG) biosynthesis by converting diacylgycerol and fatty acyl-coenzyme A into triacylglycerol. DGAT plays a fundamental role in the metabolism of cellular diacylglycerol and is important in higher eukaryotes for physiologic processes involving triacylglycerol metabolism such as intestinal absorption, lipoprotein assembly, adipose tissue formation, and lactation.
Triacylglycerol (TAG) is the essential material for mammal to maintain normal physiological function, however, too much triacylglycerol (TAG) reserve will lead to genetic obesity.
Currently, there is only one class of new drugs, (polypeptidase-4 inhibitor) was approved in the field of controlling blood sugar in people with type II diabetes. CPDs targeting lipid partitioning and lipid biosynthetic enzymes also have emerged; including inhibitors of the enzymes DGAT1 and SCD1. DGATs are the key enzymes which catalyze the final step of the triglyceride synthesis. DGAT1 gene defect and inhibition of DGAT1 can prevent obesity induced by high-fat diet and increase the sensitivity of organisms to insulin without side effect.
Hypertriglyceridemia has been identified as a major independent cardiovascular disease risk factors in the future. Diacylglycerol acyltransferase is a key enzyme in the final step of biochemical synthesis of triglycerides and therefore it has been identified as a potential therapeutic target against humanity hyperlipidemia and cardiovascular disease.
DGAT1 is an essential host factor for viral assembly, and is required for the trafficking of HCV core from endoplasmic reticulum membranes to the surface of lipid droplets (LDs) to produce infectious particle. Selective inhibition or silencing of DGAT1, but not of DGAT2, dramatically impaired the product and secretion of infectious virus, while leaving HCV RNA replication unaffected.
The global diabetes equipment and drug market reached $50.8 billion in 2011, and in accordance with market expectations, this figure will reach $98.4 billion in 2018, from 2011 to 2018, the annual growth rate of 9.9%. Chinese diabetes market reached S15 billion, the number of patients reached 39.8 million, with an annual growth rate of over 40%. The cost for treating diabetes per capita is $451, and cost for treating patients with diabetic complications is as high as $1,694. By 2025, the total number of diabetes patients in China will reach 59.3 million.
The diabetes drug market may reach $2 billion in 2017 from $1.1 billion at the end of 2009. By 2015 the diabetes and obesity market could reach $6.7 billion in China. The obesity population is 70 million in China. 14.6% of the total adult, national weight loss market capacity should be 67.7 billion yuan, however, the current weight loss products market with annual sales is less than 10 billion yuan.
Novartis is developing Pradigastat (LCQ-908, Novartis), its indications include FCS, diabetes, obesity, hyperlipoproteinemia, hypertriglyceridemia, angiocardiopathy, renal function damage or liver function damage, and it is currently in clinical trials.

Pfizer's international Patent Application WO2009016462A1, WO2010086820A1 disclosed, a series compounds, and literature “Discovery of PF-04620110: A Potent, Orally-Bioavailable Inhibitor of DGAT1, ACS Med. Chem. Lett 2011, 2, 407-412” described the compound as followed.

The activity, half-life period, solubility, pharmacokinetics and other aspects of performance of the aforesaid compounds could be improved.